Tropical Journal of Pharmaceutical Research

Original Research Article | OPEN ACCESS

Formulation and development of colon-targeted mucopenetrating metronidazole nanoparticles

Sukhbir Kaur^1,2 , R K Narang¹, Geeta Aggarwal³

¹Department of Pharmaceutics, ISF College of Pharmacy, Moga; ²IKG Punjab Technical University, Jalandhar; ³Rayatand Bahra Institute of Pharmacy, Mohali, Punjab, India.

For correspondence:- Sukhbir Kaur Email: k_sukhbir@yahoo.co.in

Received: 24 December 2016 Accepted: 21 April 2017 Published: 29 May 2017

Citation: Kaur S, Narang RK, Aggarwal G. Formulation and development of colon-targeted mucopenetrating metronidazole nanoparticles. Trop J Pharm Res 2017; 16(5):967-973 doi: 10.4314/tjpr.v16i5.1

© 2017 The authors.
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Abstract

Purpose: To formulation and develop colon-targeted mucopenetrating metronidazole nanoparticles.

Methods: Metronidazole-loaded chitosan nanoparticles with a pH-sensitive polymer, hydroxyl propyl methyl cellulose phthalate (HPMCP), were prepared by ionic gelation technique and then coated with Eudragit S100 by solvent evaporation method. The nanoparticles were optimized using one variable at a time (OVAT) approach. Further, the nanoparticles were evaluated by scanning electron microscopy (SEM) and zeta sizer, as well as for in-vitro release. Muco-adhesion was evaluated by modified bioadhesion detachment force measurement balance and muco-penetration of fluorescein isothiocyanate (FITC) labeled optimized nanoparticles was determined by microscopic technique

Results: Morphological assessment results revealed smooth, spherical particles with homogeneous distribution and polydispersity index (PDI) of 0.213. The optimized formulation showed particle size of 202 ± 27 nm, zeta potential of 26.9 ± 2.4 mV as well as and entrapment efficiency of 79 ± 5.4 %. There was significant difference in drug release between coated (8.46 ± 2.49 %) and uncoated (28.96 ± 4.04 %) nanoparticles at the 5th h in simulated gastric conditions. Muco-adhesion data revealed that uncoated nanoparticles (14.98 x 103 dyne/cm2) showed higher muco-adhesion detachment force compared to coated (12.34 x 103 dyne/cm2) nanoparticles. Muco-penetration results confirm the retention (for up to 12 h) of the developed formulation at the target site for enhanced therapeutic exposure of the entrapped drug.

Conclusion: Eudragit S100 coating of chitosan-HPMCP nanoparticles promotes efficient drug targeting and thus provides a strategy for treating mucosal infections

Keywords: Metronidazole, pH-sensitive nanoparticles, Hydroxylpropyl methylcellulose phthalate, Ionic gelation, Mucoadhesion, Mucopenetration, Intestinal infecti